Netarsudil Mesylate

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and​/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

Product information

CAS Number: 1422144-42-0

Molecular Weight: 645.74

Formula: C30H35N3O9S2

Synonym:

AR-13324

Rhopressa

Netarsudil Mesylate

Related CAS Number:

1254032-66-0 (free base)

1253952-02-1 (HCl)

Chemical Name: (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dimethanesulfonate

Smiles: CC1=CC(C)=C(C=C1)C(=O)OCC1C=CC(=CC=1)[C@@H](CN)C(=O)NC1=CC2=CC=NC=C2C=C1.CS(O)(=O)=O.CS(O)(=O)=O

InChiKey: QQDRLKRHJOAQDC-FBHGDYMESA-N

InChi: InChI=1S/C28H27N3O3.2CH4O3S/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24;2*1-5(2,3)4/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32);2*1H3,(H,2,3,4)/t26-;;/m1../s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Mehran NA, Sinha S, Razeghinejad R. New glaucoma medications: latanoprostene bunod, netarsudil, and fixed combination netarsudil-latanoprost. Eye (Lond). 2019 Nov 6. doi: 10.1038/s41433-019-0671-0. [Epub ahead of print] Review. PubMed PMID: 31695162.
2. Sinha S, Lee D, Kolomeyer NN, Myers JS, Razeghinejad R. Fixed combination netarsudil-latanoprost for the treatment of glaucoma and ocular hypertension. Expert Opin Pharmacother. 2019 Oct 30:1-7. doi: 10.1080/14656566.2019.1685499. [Epub ahead of print] PubMed PMID: 31663782.
3. Radell JE, Serle JB. Netarsudil/latanoprost fixed-dose combination for the treatment of open-angle glaucoma or ocular hypertension. Drugs Today (Barc). 2019 Sep;55(9):563-574. doi: 10.1358/dot.2019.55.9.3039670. PubMed PMID: 31584573.

Products are for research use only. Not for human use.